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Novel 3-Aminopyrazole Inhibitors of MK-2 Discovered by Scaffold Hopping Strategy

Velcicky, Juraj and Feifel, Roland and Hawtin, Stuart and Heng, Richard and Huppertz, Christine and Koch, Guido and Kroemer, Markus and Moebitz, Henrik and Revesz, Laszlo and Scheufler, Clemens and Schlapbach, Achim (2009) Novel 3-Aminopyrazole Inhibitors of MK-2 Discovered by Scaffold Hopping Strategy. Bioorganic and Medicinal Chemistry Letters, 20 (3). pp. 1293-1297. ISSN 0960-894X

Abstract

New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFa release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFa release in vivo.

Item Type: Article
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Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: MK2; TNFα-inhibition; 3-Aminopyrazole; Scaffold hopping; Induced-fit; X-ray
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Date Deposited: 13 Oct 2015 13:17
Last Modified: 13 Oct 2015 13:17
URI: https://oak.novartis.com/id/eprint/1178

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